1-oxa-5-aza-bicyclo (4.2.0) Octanes (including Unsaturated) Patents (Class 514/210.08)
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Patent number: 8592454Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.Type: GrantFiled: September 18, 2009Date of Patent: November 26, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Junya Shirai, Hideyuki Sugiyama, Taku Kamei, Hironobu Maezaki
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Patent number: 8569281Abstract: The present invention relates to substituted pyrazolopyridine compounds, and pharmaceutically acceptable salts or esters thereof. The present invention further relates to therapeutic uses of pharmaceutical compositions comprising the substituted pyrazolopyridine compounds, for example, in cancer and neurodegenerative diseases.Type: GrantFiled: September 21, 2011Date of Patent: October 29, 2013Assignees: Medical Research Council Technology, Genentech, Inc.Inventors: Bryan K. Chan, Huifen Chen, Anthony Estrada, Daniel Shore, Zachary Sweeney, Edward Giles McIver
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Patent number: 8529935Abstract: The present invention relates to hydrogels endowed with antibacterial properties, to be used for injection in damaged bones or in the production of antibacterial coatings of prostheses for implant in the human or animal body, obtained by loading with antibacterial agents hydrogels formed by derivatives of hyaluronic acid; the invention also relates to a kit of parts for producing the antibacterial hydrogels.Type: GrantFiled: January 29, 2010Date of Patent: September 10, 2013Assignees: Mero S.R.L., Novagenit S.R.L.Inventors: Gaetano Giammona, Giovanna Pitarresi, Fabio Palumbo, Carlo Luca Romano, Enzo Meani, Edgardo Cremascoli
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Publication number: 20130131032Abstract: A method for improving sexual function is described. A mammal suffering from sexual dysfunction or otherwise in need of enhanced sexual function is administered a compound selected from those that are capable of inhibiting the activity of ?-lactams, penicillin-binding protein, carboxypeptidase. Such compounds, including particularly ?-lactam ring-containing compounds, can be used to formulate pharmaceutical formulations useful for improving sexual function.Type: ApplicationFiled: January 25, 2013Publication date: May 23, 2013Applicant: Revaax Pharmaceuticals, LLCInventor: Revaax Pharmaceuticals, LLC
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Publication number: 20130102583Abstract: A compound of the formula: wherein X is —N?, —CH?, or the like; W is —CH2— or the like; U is —S— or the like; R1 and R2 are each independently hydrogen, halogen, optionally substituted lower alkyl, or the like; R3 is hydrogen or the like; each R4 is independently hydrogen, halogen, or the like; m is an integer from 0 to 2; Q is a single bond, or the like; G is —C(?O)—, or the like; D is a single bond, —NH—, or the like; and E is a cyclic quaternary ammonium group, or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: April 4, 2011Publication date: April 25, 2013Applicant: SHIONOGI & CO., LTD.Inventors: Shinya Hisakawa, Yasushi Hasegawa, Toshiaki Aoki, Hiroki Kusano, Masayuki Sano, Jun Sato, Kenji Yamawaki
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Publication number: 20120172292Abstract: This invention discloses a method for enhancing the efficacy of antimicrobial, anti-protozoa and anti-cancer treatments by co-administering an inhibitor of endogenous NO production and/or NO scavenger.Type: ApplicationFiled: September 10, 2010Publication date: July 5, 2012Applicant: NEW YORK UNIVERSITYInventors: Evgeny A. Nudler, Ivan Gusarov
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Publication number: 20110294774Abstract: The present invention provides a pharmaceutical composition useful for treating bacterial infections in humans and animals which comprises administering to a human or animal in need thereof, an antibacterially effective combination of a ?-lactam antibiotic and an inhibitor of any bacterial peptidoglycan biosynthesis enzyme, especially GlmU, GlmU, MurA, MurB, MurC, MurD, MurE, MurF, MurG, MraY, and UppS.Type: ApplicationFiled: May 6, 2011Publication date: December 1, 2011Applicant: TRIUS THERAPEUTICSInventors: Vickie Brown-Driver, Kedar GC, John M. Finn, Robert Haselbeck, Mark Hilgers, Karen Shaw, Mark Stidham
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Publication number: 20110280921Abstract: The present invention relates to hydrogels endowed with antibacterial properties, to be used for injection in damaged bones or in the production of antibacterial coatings of prostheses for implant in the human or animal body, obtained by loading with antibacterial agents hydrogels formed by derivatives of hyaluronic acid; the invention also relates to a kit of parts for producing the antibacterial hydrogels.Type: ApplicationFiled: January 29, 2010Publication date: November 17, 2011Applicants: NOVAGENIT S.R.L., MERO S.R.LInventors: Gaetano Giammona, Giovanna Pitarresi, Fabio Palumbo, Carlo Luca Romano, Enzo Meani, Edgardo Cremascoli
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Publication number: 20110257147Abstract: A method for improving sexual function is described. A mammal suffering from sexual dysfunction or otherwise in need of enhanced sexual function is administered a compound selected from those that are capable of inhibiting the activity of ?-lactams, penicillin-binding protein, carboxypeptidase. Such compounds, including particularly ?-lactam ring-containing compounds, can be used to formulate pharmaceutical formulations useful for improving sexual function.Type: ApplicationFiled: June 27, 2011Publication date: October 20, 2011Applicant: Revaax Pharmaceuticals, LLCInventor: Gary A. Koppel
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Publication number: 20110046101Abstract: The present invention relates to broad spectrum ?-lactamase inhibitors. More particularly, the invention relates to inhibitors of Class B metallo (MBL) and Class D (OXA) ?-lactamases. A method of treating a bacterial infection is provided, wherein the method comprises administering to a mammalian patient in need of such treatment a compound of formula (I) wherein R1 is selected from R2 is selected from with certain provisos as herein defined; in combination with a pharmaceutically acceptable ?-lactam antibiotic in an amount which is effective for treating the bacterial infection.Type: ApplicationFiled: March 17, 2008Publication date: February 24, 2011Inventors: Gary I. Dmitrienko, Jarrod W. Johnson, Timothy R. Ramadhar, Thammaiah Viswanatha, Sundaramma Viswanatha
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Patent number: 7842683Abstract: Administration of ?-Lactam compounds, including ?-lactam antibiotics and ?-lactamase inhibitors provides significant neurotropic effects in warm-blooded vertebrates evidence inter alia by anxiolytic and anti-aggressive behavior modification and enhanced cognition. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.Type: GrantFiled: January 23, 2008Date of Patent: November 30, 2010Assignee: Revaax Pharmaceuticals, LLCInventor: Gary A. Koppel
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Publication number: 20100249090Abstract: Neurotherapeutically effective pharmaceutical compositions are described that include carboxypeptidase E inhibitors. One class of carboxypeptidase E inhibitors found to exhibit significant neurotropic activity are ?-lactam compounds, particularly penam and cephem ?-lactam antibiotics and non-antibiotic derivatives thereof.Type: ApplicationFiled: May 13, 2010Publication date: September 30, 2010Inventors: Gary A. Koppel, Michael O. Chaney
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Publication number: 20100040548Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.Type: ApplicationFiled: June 10, 2009Publication date: February 18, 2010Inventor: Chongxi Yu
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Publication number: 20090253676Abstract: Compounds of Formula (I): wherein: R1 is hydroxymethyl; R2 is selected from —C(O)NR4R5, —SO2NR4R5, —S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro-drug or solvate thereof, are described.Type: ApplicationFiled: December 16, 2008Publication date: October 8, 2009Applicant: AstraZeneca ABInventors: Craig Johnstone, Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Publication number: 20080312203Abstract: The present invention provides a compound of formula I wherein one of A and B is hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X is O, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.Type: ApplicationFiled: August 21, 2008Publication date: December 18, 2008Applicant: WyethInventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo Dos Santos, Fuk-Wah Sum, Yang-I Lin
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Patent number: 7439253Abstract: The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a method for preparing these compounds, and to their use as medicaments, in particular as antibacterials and ?-lactamase inhibitors.Type: GrantFiled: December 4, 2003Date of Patent: October 21, 2008Assignee: NovexelInventors: Maxime Lampilas, Branislav Musicki, Michel Klich, David Alan Rowlands
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Publication number: 20080200447Abstract: Administration of ?-Lactam compounds, including ?-lactam antibiotics and ?-lactamase inhibitors provides significant neurotropic effects in warm-blooded vertebrates evidence inter alia by anxiolytic and anti-aggressive behavior modification and enhanced cognition. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.Type: ApplicationFiled: January 23, 2008Publication date: August 21, 2008Applicant: REVAAX PHARMACEUTICALS, LLCInventor: Gary A. Koppel
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Publication number: 20080146535Abstract: The present invention relates to pharmaceutical compositions of carbocephem antibiotics with ?-lactamase inhibitors useful for the treatment of bacterial infections, in particular infections caused by bacteria that express ?-lactamases as a mechanism of resistance to ?-lactam antibiotics.Type: ApplicationFiled: September 2, 2005Publication date: June 19, 2008Inventors: Tomasz Glinka, George Miller
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Patent number: 6627625Abstract: Administration of &bgr;-lactam compounds including &bgr;-lactam antibiotics and &bgr;-lactamase inhibitors provides significant neurotropic effects in warm-blooded vertebrates evidenced inter alia by anxiolytic and anti-aggressive behavior modification and enhanced cognition. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.Type: GrantFiled: August 16, 2000Date of Patent: September 30, 2003Assignee: Revaax Pharmaceuticals, LLCInventor: Gary A. Koppel
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Patent number: 6514962Abstract: Stabilized preparations which contain a &bgr;-lactam antibiotic having an esterified carboxyl group attached directly to the mother nucleus, an oil and a phosphate.Type: GrantFiled: February 5, 2001Date of Patent: February 4, 2003Assignee: Takeda Schering-Plough Animal Health K.K.Inventors: Hatsuo Shibatani, Tomoyasu Nakamura
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Patent number: 6489319Abstract: Administration of inhibitors of carboxypeptidase E provides significant neurotropic effects in warm-blooded vertebrates evidenced inter alia by anxiolytic and anti-aggressive behavior and enhanced cognition. Certain &bgr;-Lactam antibiotics, most significantly, certain 1-oxa-1-dethia cephems with blood brain barrier transport, exhibit potent therapeutic neurologic activity.Type: GrantFiled: February 14, 2001Date of Patent: December 3, 2002Assignee: Revaax Pharmaceuticals, LLCInventors: Gary A. Koppel, Michael O. Chaney
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Patent number: 6475522Abstract: Synthetic polymer compositions contain antibiotics as antidegradants. Antibiotics from classes of glycopeptides and &bgr;-lactams have been found to prevent or inhibit synthetic polymer degradation.Type: GrantFiled: August 30, 2000Date of Patent: November 5, 2002Assignee: Hammond Group, Inc.Inventor: Richard F. Grossman